- A New Biginelli Reaction Procedure using Potassium Hydrogen Sulfate as the Promoter for an Efficient Synthesis of 3,4-Dihydropyrimidin-2(1H)-one
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Simple and improved conditions have been found to carry out the Biginelli reaction for the synthesis of 3,4-dihydropyrimidin-2(1H)-one derivatives. This synthesis was performed using potassium hydrogen sulfate as the promoter in ethylene glycol solution.
- Tu, Shujiang,Fang, Fang,Zhu, Songlei,Li, Tuanjie,Zhang, Xiaojing,Zhuang, Qiya
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- Dihydropyrimidinones: Efficient one-pot green synthesis using Montmorillonite-KSF and evaluation of their cytotoxic activity
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A simple, efficient, cost-effective, recyclable and green approach has been developed for the synthesis of new dihydropyrimidinone analogs via the Biginelli reaction. The methodology involves a multicomponent reaction catalyzed by "HPA-Montmorillonite-KSF"as a reusable and heterogeneous catalyst. This method gives an efficient and much improved modification of the original Biginelli reaction, in terms of yield and short reaction times under solvent free conditions. All the derivatives were subjected to cytotoxicity screening against a panel of four different human cancer cell lines viz. colon (Colo-205), prostate (PC-3), leukemia (THP-1) and lung (A549) to check their effect on percentage growth. MTT [3-(4,5-dimethylthiazol-yl)-diphenyl tetrazoliumbromide] cytotoxicity assay was employed to check IC50 values. Of the synthesized analogs, 16a showed the best activity with IC50 of 7.1 ± 0.8, 13.1 ± 1.4, 13.8 ± 0.9 and 14.7 ± 1.1 μM against lung (A549), leukemia (THP-1), prostate (PC-3) and colon (Colo-205) cancer lines, respectively. The 16a analog was further checked for its effect on cancer cell properties through clonogenic (colony formation) and scratch motility (wound healing) assays and thereby was found that it reduced both the colony formation and migratory properties of the lung cancer cell line (A549). Further, molecular docking studies were performed with 16a to show its binding mode. This journal is
- Alharthi, Fahad A.,Alsalme, Ali,Dar, Bashir A.,Farooq, Saleem,Hamid, Abid,Hussain, Aashiq,Koul, S.
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p. 42221 - 42234
(2020/12/09)
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- Polyaniline Supported FeCl3: An Effective Heterogeneous Catalyst for Biginelli Reaction
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Abstract: Polyaniline supported FeCl3 is prepared and tested as an efficient heterogeneous Lewis acidic catalyst for the Biginelli reaction. The catalyst PANI–FeCl3 shows excellent activity in the synthesis of dihydropyrimidinones fr
- Patel, Heta A.,Sawant, Aishwarya M.,Rao, Vandana J.,Patel, Arun L.,Bedekar, Ashutosh V.
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p. 2306 - 2312
(2017/08/22)
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- One-pot Synthesis of 1,2,3,4-Tetrahydropyrimidin-2(1H)-thione Derivatives and their Biological Activity
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2-Thioxo/oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate derivatives 2a, 2b, 2c, 2d were prepared by the reaction of ethyl acetoacetate and thiourea or urea with aldehydes using NH4Cl as a catalyst. Compounds 2a and 2c reacted with mono and biha
- Salem, Mounir A. I.,Marzouk, Magda I.,Salem, Marwa S.,Alshibani, Ghazala A.
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p. 545 - 557
(2016/04/19)
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- Polyphosphoric acid catalyst for the one-pot synthesis of 3,4-dihydropyrimidin- 2(1H)-ones by grinding under solvent-free conditions
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3,4-Dihydropyrimidin-2-(1H)-ones have been obtained, in high yield, by grinding ternary mixture of different substituted aromatic aldehydes, ethyl acetoacetate and urea, in the presence of polyphosphoric acid, under solventless conditions. The facile reac
- Zhao, Ying,Zhao, Yongguang,Zhang, Jianping,Liu, Hongmei,Liang, Liman
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p. 139 - 141
(2015/01/30)
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- Propylphosphonic anhydride-catalyzed tandem approach for biginelli reaction starting from alcohols
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An efficient and highly convergent route to dihydropyrimidinones (DHPMs) has been developed by one-pot threecomponent oxidative cyclocondensation of a variety of alcohols, β-ketoesters/β-oxodithioester and urea in the presence of T3Pμ/ DMSO. This new appr
- Revanna, Cigalli N.,Raghavendra, Goravanalli M.,Vijay, T. A. Jenifer,Rangappa, Kanchugarakoppal S.,Badregowda, Doddamedur G.,Mantelingu, Kempegowda
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supporting information
p. 178 - 180
(2014/03/21)
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- Graphite catalyzed solvent free synthesis of dihydropyrimidin-2(1H)-ones/ thiones and their antidiabetic activity
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A solvent free three component condensation reaction between an aldehyde, ethyl acetoacetate and urea catalyzed by graphite, a green catalyst is described for the synthesis of dihydropyrimidin-2(1H)-ones. This protocol is scalable and the catalyst is reus
- Dhumaskar, Kashinath L.,Meena, Surya Nandan,Ghadi, Sanjeev C.,Tilve, Santosh G.
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p. 2897 - 2899
(2014/06/10)
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- Silica gel supported bismuth nitrate pentahydrate: A highly active catalyst under solvent free conditions towards the synthesis of dihydropyrimidin-2(1H)- ones and their sulphur analogues
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Silica gel supported bismuth nitrate pentahydrate has been shown to be an efficient catalyst for the Biginelli reaction. The main advantages of the catalyst include short reaction time and high yield of the products. This observation has been confirmed by
- Hingane, Dattatray G.,Shumaila, Abdullah M.A.,Kusurkar, Radhika S.
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p. 1161 - 1165
(2013/09/24)
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- The biginelli reaction with an imidazolium-tagged recyclable iron catalyst: Kinetics, mechanism, and antitumoral activity
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The present work describes the synthesis, characterization, and application of a new ion-tagged iron catalyst. The catalyst was employed in the Biginelli reaction with impressive performance. High yields have been achieved when the reaction was carried ou
- Ramos, Luciana M.,Guido, Bruna C.,Nobrega, Catharine C.,Corrêa, José R.,Silva, Rafael G.,De Oliveira, Heibbe C. B.,Gomes, Alexandre F.,Gozzo, Fábio C.,Neto, Brenno A. D.
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supporting information
p. 4156 - 4168
(2013/05/08)
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- Iron(III) tosylate catalyzed synthesis of 3,4-dihydropyrimidin-2(1H)-ones/ thiones via the Biginelli reaction
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The synthesis of dihydropyrimidinones and dihydropyrimidine thiones has attracted interest due to their biological activities. A common method for their synthesis is the Biginelli reaction, which is a one-pot condensation of an aryl aldehyde, urea (or thi
- Starcevich, Jacob T.,Laughlin, Thomas J.,Mohan, Ram S.
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p. 983 - 985
(2013/02/25)
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- Trifluoroethanol as a metal-free, homogeneous, and recyclable medium for the efficient one-pot synthesis of dihydropyrimidones
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Trifluoroethanol is an efficient and recyclable medium in promoting one-pot, three-component condensation reactions of b-ketoesters, aldehydes, and urea (or thiourea) to afford the corresponding dihydropyrimidones in good yields. This protocol does not re
- Rashmi,Sandhya,Raghava,Kumara,Mantelingu,Rangappa
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experimental part
p. 424 - 433
(2011/11/29)
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- One-pot synthesis of dihydropyrimidiones via environmentally friendly enzyme-catalyzed Biginelli reaction
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A novel enzyme-catalyzed Biginelli reaction of acetoacetate, aromatic aldehyde and urea (thiourea) was described. Great acceleration of the one-pot multicomponent reaction was observed by the aid of enzymes. Various dihydropyrimidiones were prepared in go
- Li, Wanmei,Zhou, Guobin,Zhang, Pengfei,Lai, Yifeng,Xu, Shifu
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experimental part
p. 2067 - 2077
(2011/10/13)
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- Synthesis of dihydropyrimidin-2-one/thione library and cytotoxic activity against the human U138-MG and Rat C6 glioma cell lines
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Two series of 4-aryl-3,4-dihydropyrimidin-2(1H)-(thio)ones including monastrol (1a), have been synthesized by an environment-friendly methodology based on the combined use of citric acid or oxalic acid and TEOF (triethylorthoformate). The library was eval
- Canto, Ro?mulo F.S.,Bernardi, Andressa,Battastini, Ana Maria O.,Russowsky, Dennis,Eifler-Lima, Vera Lucia
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experimental part
p. 1379 - 1388
(2012/04/17)
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- P-Sulfonic acid calixarenes as efficient and reusable organocatalysts for the synthesis of 3,4-dihydropyrimidin-2(1H)-ones/-thiones
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A new and efficient methodology is proposed for obtaining 3,4-dihydropyrimidin-2(1H)-ones/-thiones through Biginelli reactions. It is based on the use of less than the stoichiometric amount ofp-sulfonic acid calixarenes as organocatalysts. A number of aro
- Da Silva, Daniel L.,Fernandes, Sergio A.,Sabino, Ad?o A.,De Fá, ?ngelo
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experimental part
p. 6328 - 6330
(2011/12/22)
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- Ionic liquid catalyzed synthesis of 3,4-dihydropyrimidin-2(1H)-ones under microwave irradiation
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An effective synthesis of 3,4-dihydropyrimidin-2(1H)-one derivatives using ionic liquid 1-n-butyl-3-methylimmidazolium hexafluorophosphate ([bmim]PF 6) as the catalyst from aldehydes, 1,3-dicarbonyl compounds and urea (thiourea) under microwave
- Wang, Qin,Pei, Wen
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experimental part
p. 806 - 808
(2011/10/12)
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- Synthesis of 3,4-dihydropyrimidin-2(1H)-ones Using Ce(SO4) 2-SiO2 as a heterogeneous and recyclable catalyst
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A simple and efficient synthesis of 3,4-dihydropyrimidinones or thiones is described, using silica-supported ceric sulfate [Ce(SO4) 2-SiO2] as a heterogeneous catalyst from an aldehyde, 1,3-dicarbonyl compound, and urea or
- Pei, Wen,Wang, Qin
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experimental part
p. 1209 - 1215
(2010/05/17)
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- Three component reaction: An efficient synthesis of 3,4-dihydropyrimidin-2(1H)-ones and thiones using heterogeneous catalyst
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Fluoroboric acid supported on silica gel (HBF4-SiO2) catalyzes efficiently the three component condensation of an aldehyde, a 1,3-dicarbonyl compound and urea or thiourea to afford the corresponding 3,4-dihydropyrimidin-2(1H)-ones an
- Kamble, Vinod Tribhuvannathji,Muley, Dnyanoba Baburao,Atkore, Sandeep Tukaram,Dakore, Sharad Digambarrao
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experimental part
p. 388 - 392
(2010/10/02)
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- VOSO4-catalyzed biginelli condensation: An efficient synthesis of dihydro-1h-pyrimidine-2-thione/one and octahydro-2,5-quinazolinedione
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The three component condensation of an aldehyde 1, urea/thiourea 2 and β-ketoester 3/dimidone 7 in the presence of a catalytic amount of VOSO 4 is disclosed for the synthesis of 3,4-dihydro-1 H-pyrimidine-2-thione/one (DHPMs) 4 and octahydro-2,
- Reddy, Ch Sanjecva,Raghu,Nagaraj
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experimental part
p. 1178 - 1182
(2009/12/26)
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- Simple and efficient one-pot synthesis of 3,4-dihydro-2-pyridones via solid-supported Bi(III)nitrate catalyzed double Michael addition-azaannulation
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(Chemical Equation Presented) 4-Aryl-5-carboethoxy-6-methyl-2,3-dihydro-2- pyridones were obtained, in high yield, by heating ternary mixtures of appropriate aldehydes, ethylacetoacetate and compounds possessing NH 2-C=X functionality, in prese
- Singh, Jagjeet,Koui, Summon,Pannu, Ajay P. S.,Sharma, Rattan L.,Razdan, Tej K.
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p. 349 - 357
(2008/09/20)
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- Synthesis and in vitro evaluation of the antifungal activities of dihydropyrimidinones
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Copper (II) chloride in the absence of any solvent, efficiently catalyses the synthesis of dihydropyrimidinones (80-96% yields) by the Biginelli reaction. Six compounds were selected and examined their antifungal activities against the radial growth of th
- Singh, Okram Mukherjee,Singh, Sarangthem Joychandra,Devi, Mutum Babita,Devi, Laitonjam Nalini,Singh, Nameirakpam Irabanta,Lee, Sang-Gyeong
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body text
p. 6462 - 6467
(2009/10/01)
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- Biginelli reactions in molten ammonium bromides
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3,4-Dihydropyrimidin-2(1 H)-ones were synthesized in good yields by solvent-free one-pot three-component Biginelli condensation in the presence of molten tetrabutylammonium bromide or ammonium bromide as catalyst,irrespective of the presence of electron donating or electron withdrawing groups aromatic aldehydes.
- De Souza, Andrea Luzia F.,De Oliveira, Mara Rita P.,Teixeira Da Silva, Emerson,Lopez Fernandeza, Tatiana,Antunesa
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experimental part
p. 357 - 361
(2009/05/31)
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- One-pot synthesis of 3,4-dihydropyrimidin-2(1H)-ones catalyzed by acidic ionic liquid
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3,4-Dihydropyrimidin-2(1H)-ones have been synthesized via one-pot reaction of aromatic aldehydes, ethyl acetoacetate and urea or thiourea catalyzed by room temperature ionic liquid [hmim]HSO4. It has been observed that the proposed method is fa
- Ma, Jing-Jun,Zang, Xiao-Huan,Zhou, Xin,Wang, Chun,Li, Jing-Ci,Li, Qing
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p. 2045 - 2048
(2008/09/18)
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- Solvent-free approach to 3,4-dihydropyrimidin-2(1H)-(thio)ones: Biginelli reaction catalyzed by a Wells-Dawson reusable heteropolyacid
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The Biginelli reaction is performed in an efficient, simple, solvent-free procedure, using a small amount of H6P2W18O62 · 24H2O, a reusable heteropolyacid catalyst with Wells-Dawson structure. Both aromatic and aliphatic aldehydes, and different β-dicarbo
- Romanelli, Gustavo P.,Sathicq, Angel G.,Autino, Juan C.,Baronetti, Graciela,Thomas, Horacio J.
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p. 3907 - 3916
(2008/03/13)
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- Zirconium oxychloride as a new and efficient catalyst for the synthesis of 3,4-dihydropyrimidine-2(1h)-thione/one under solvent-free microwave irradiation conditions
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ZrOCl2 has been found to be an efficient catalyst for the one-pot synthesis of 3,4-dihydropyrimidine-2(1H)-thione/one, from β-ketoester, aldehyde and (thio)urea under solvent-free microwave irradiation conditions. The beneficial effects of ZrOC
- Reddy, Ch. Sanjeeva,Nagaraj
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- SNCL2-catalyzed synthesis of dihydropyrimidinones under solvent-free conditions
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A simple, efficient and practical green synthetic route to the Biginelli cyclocondensation reaction using Stannous (II) Chloride Dihydrate as the catalyst is described under solvent free conditions to yield dihydropyrimidinones in high yields.
- Singh, Okram M.,Singh, M. Lokeshwar,Singh, S. Joychandra
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p. 277 - 282
(2008/03/13)
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- Sodium tetrafluoroborate as a new and highly efficient catalyst for one-pot synthesis of 3,4-dihydropyrimidin-2(1H)-ones and thiones
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Sodium tetrafluoroborate (NaBF4) is found to catalyze the three component condensation of an aldehyde, 1,3-dicarbonyl compound and urea or thiourea to afford the corresponding 3,4-dihydropyrimidin-2(1H)-ones and thiones in high yields. This met
- Bandgar,Kamble,Bavikar,Dhavane, Abasaheb
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p. 263 - 266
(2008/02/10)
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- Calcium chloride catalyzed three component, one-pot condensation reaction: An efficient synthesis of 3,4-dihydropyrimidin-2(1H)-ones
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CaCl2 is an efficient, inexpensive and readily available catalyst for the three component, one-pot condensation reaction of an aldehyde, β-ketoester and urea in refluxing ethanol to afford the corresponding dihydropyrimidinones in high yield. T
- Gangadasu,Narender,Raju, B. China,Rao, V. Jayathirtha
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p. 1259 - 1263
(2007/10/03)
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- Synthesis and differential antiproliferative activity of Biginelli compounds against cancer cell lines: Monastrol, oxo-monastrol and oxygenated analogues
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The synthesis and differential antiproliferative activity of monastrol (1a), oxo-monastrol (1b) and eight oxygenated derivatives 3a,b-6a,b on seven human cancer cell lines are described. For all evaluated cell lines, monastrol (1a) was shown to be more ac
- Russowsky, Dennis,Canto, Romulo F.S.,Sanches, Sergio A.A.,D'Oca, Marcelo G.M.,de Fatima, Angelo,Pilli, Ronaldo A.,Kohn, Luciana K.,Antonio, Marcia A.,de Carvalho, Joao Ernesto
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p. 173 - 182
(2008/02/09)
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- Scandium(III) triflate as an efficient and reusable catalyst for synthesis of 3,4-dihydropyrimidin-2(1H)-ones
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Sc(III) triflate efficiently catalyzes the three-component condensation reaction of an aldehyde, a β-ketoester, and urea in refluxing acetonitrile to afford the corresponding 3,4-dihydropyrimidin-2(1H)-ones in excellent yields. The catalyst can be recover
- De, Surya K.,Gibbs, Richard A.
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p. 2645 - 2651
(2007/10/03)
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- A one-pot synthesis of 3,4-dihydropyrimidin-2-(IH)-onesfrom primary alcohols promoted by Bi(NO3)3.5H2O in two different media: Organic solvent and ionic liquid
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A new, simple and efficient procedure for the one-pot conversion of alcohols instead of aldehydes to the corresponding 3,4-dihydropyrimidin-2(1H)-ones (DHPMs) with Bi(NO3)3.5H2O as a commercially available, inexpensive, st
- Khosropour, Ahmad R.,Khodaei, Mohammd M.,Beygzadch, Mojtaba,Jokar, Mahbubeh
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p. 767 - 773
(2007/10/03)
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- NbCl5-catalyzed rapid and efficient synthesis of 3,4-dihydropyrimidinones under ambient conditions
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Three-component condensation of an aldehyde, 1,3-dicarbonyl compound and urea or thiourea proceeds smoothly at room temperature in the presence of 5 mol % of NbCl5 under extremely mild conditions to afford the corresponding 3,4-dihydropyrimidin
- Yadav,Reddy,Naidu, Jaishri J.,Sadashiv
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p. 926 - 927
(2007/10/03)
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- An efficient one-pot synthesis of 3,4-dihydropyrimidin-2-ones catalyzed by methanesulfonic acid
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An efficient synthesis of 3,4-dihydropyrimidin-2-ones (DHPMs) from the aldehydes, β-ketoesters, and urea in ethanol using methanesulfonic acid (CH3SO3H) as the catalyst is described. Compared with the classical Biginelli reaction con
- Jin, Tong-Shou,Wang, Huan-Xin,Xing, Chun-Yong,Li, Xiao-Liu,Li, Tong-Shuang
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p. 3009 - 3016
(2007/10/03)
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- A New Biginelli Reaction Procedure Using Potassium Hydrogen Sulfate as the Promoter for an Efficient Synthesis of 3,4-Dihydropyrimidin-2(1H)-one
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Simple and improved conditions have been found to carry out the Biginelli reaction for the synthesis of 3,4-dihydropyrimidin-2(1H)-one derivatives. This synthesis was performed using potassium hydrogen sulfate as the promoter in glycol solution. Compared
- Tu, Shujiang,Fang, Fang,Zhu, Songlei,Li, Tuanjie,Zhang, Xiaojing,Zhuang, Qiya
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p. 537 - 539
(2007/10/03)
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- A highly efficient solvent-free synthesis of dihydropyrimidinones catalyzed by zinc chloride
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Dihydropyrimidinones are prepared from zinc chloride (20 mol%) catalyzed Biginelli condensation of an aldehyde, 1,3-dicarbonyl compounds and urea or thiourea at 80°C for short time under solvent-free conditions in high yields.
- Sun, Qi,Wang, Yi-Qiang,Ge, Ze-Mei,Cheng, Tie-Ming,Li, Run-Tao
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p. 1047 - 1051
(2007/10/03)
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- Iodine catalyzed one-pot synthesis of 3,4-dihydropyrimidin-2(1H)-ones and thiones: A simple and efficient procedure for the Biginelli reaction
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Iodine efficiently catalyzes the Biginelli reaction. This procedure involves a one-pot three-component cyclocondensation of aldehydes, 1,3-dicarbonyl compounds and urea or thiourea to afford the corresponding 3,4-dihydropyrimidin-2(1H)-ones or thiones in
- Srinivas,Das, Biswanath
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p. 2091 - 2093
(2007/10/03)
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- Phosphotungstic acid catalysed one-pot synthesis of 5-alkoxycarbonyl-4-aryl-3,4-dihydropyrimidin-2-ones
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5-Alkoxycarbonyl-4-aryl-3,4-dihydropyrimidin-2-ones are synthesised by the one-pot reactions of aldehydes, β-ketoesters and urea using a catalytic amount of phosphotungstic acid (PTA) in ethanol. The modified Biginelli cyclocondensation not only shortens
- Jin, Tong-Shou,Xiao, Jin-Chong,Chen, Van-Xue,Li, Tong-Shuang
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p. 190 - 191
(2007/10/03)
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- One-pot synthesis of dihydropyrimidinones catalysed by lithium bromide: An improved procedure for the Biginelli reaction
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LiBr catalyses efficiently the three component condensation reaction of an aldehyde, a β-ketoester and urea in refluxing acetonitrile to afford the corresponding dihydropyrimidinones in high yield.
- Maiti, Gourhari,Kundu, Pradip,Guin, Chandrani
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p. 2757 - 2758
(2007/10/03)
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- One-pot synthesis of 3,4-dihydropyrimidin-2(1H)-ones using boric acid as catalyst
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A simple effective synthesis of 3,4-dihydropyrimidin-2(1H)-one derivatives, using boric acid as catalyst, from aromatic aldehydes, 1,3-dicarbonyl compounds and urea in glacial acetic acid is described. Compared with the classical Biginelli reaction condit
- Tu, Shujang,Fang, Fang,Miao, Chunbao,Jiang, Hong,Feng, Youjian,Shi, Daqing,Wang, Xiangshan
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p. 6153 - 6155
(2007/10/03)
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- Clay catalysed synthesis of dihydropyrimidinones under solvent-free conditions
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A fast and high yielding one-pot synthesis of 3,4-dihydropyrimidin-2(1H)-ones from β-keto esters, urea and various aliphatic and aromatic aldehydes using montmorillonite KSF clay as a catalyst in solvent-free condition under microwave irradiation is descr
- Mitra, Alok Kumar,Banerjee, Krishna
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p. 1509 - 1511
(2007/10/03)
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- One-pot synthesis of 3,4-dihydropyrimidin-2(1H)-ones using cadmium sulfate as catalyst
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A simple effective synthesis of 3,4-dihydropyrimidin-2(1H)-one derivatives from aromatic aldehydes, 1,3-dicarbonyl compounds and urea in glacical acetic acid using cadmium sulfate as catalyst is described and compared with the classical Biginelli reaction
- Tu, Shujang,Fang, Fang,Miao, Chunbao,Jiang, Hong,Shi, Daqing,Wang, Xiangshan
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p. 544 - 545
(2007/10/03)
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- Iron(III)-catalyzed synthesis of dihydropyrimidinones in solvent-free condition under microwave irradiation
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An efficient and fast synthesis of 3,4-dihydropyrimidinones from the aldehyde, β-keto ester and urea using ferric chloride hexahydrate as catalyst in solvent-free condition under microwave irradiation is described.
- Banerjee, Krishna,Mitra, Alok Kumar
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- Cu(OTf)2: A reusable catalyst for high-yield synthesis of 3,4-dihydropyrimidin-2(1H)-ones
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Copper(II) triflate catalyzes efficiently the three-component condensation reaction of an aldehyde, β-ketoester and urea in acetonitrile to afford the corresponding 3,4-dihydropyrimidin-2(1H)-ones in high yields. The catalyst exhibited remarkable reusable activity.
- Paraskar,Dewkar,Sudalai
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p. 3305 - 3308
(2007/10/03)
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- Oxalic acid - A new catalyst for the syntheses of dihydropyrimidinones in solvent-free condition
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High yielding and fast one-pot synthesis of 3,4-dihydropyrimidin-2(1H)-ones from β-ketoesters, urea and various aldehydes using oxalic acid as a catalyst in solvent-free condition under microwave irradiation is reported.
- Mitra, Alok Kumar,Banerjee, Sajal Kumar
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p. 1175 - 1178
(2007/10/03)
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- A convenient ferric chloride catalyzed synthesis of 5-alkoxycarbonyl-4-aryl-3,4-dihydropyrimidin-2(1H)-ones under microwave irradiation
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A series of ethyl 4-aryl-6-methyl-1,2,3,4-tetrahydropyrimidin-2-one-5-carboxylates 4 were synthesized by the condensation of aromatic aldehydes, ethyl acetoacetate and urea in the presence of ferric chloride hexahydrate under microwave irradiation. The reactions were completed in 4-6 min with 87-92% yield.
- Tu, Shu-Jiang,Zhou, Jian-Feng,Cai, Pei-Jun,Wang, Hai,Feng, Jun-Cai
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p. 147 - 151
(2007/10/03)
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- A practical and green approach towards synthesis of dihydropyrimidinones without any solvent or catalyst
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A simple, efficient, green, and cost-effective procedure has been developed for the synthesis of dihydropyrimidinones by a solvent-free and catalyst-free Biginelli's condensation of 1,3-dicarbonyl compound, aldehyde, and urea. This approach of direct reaction in neat without solvent and catalyst shows a new direction in green synthesis.
- Ranu, Brindaban C.,Hajra, Alakananda,Dey, Suvendu S.
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p. 817 - 818
(2013/09/06)
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- Catalysis of the Biginelli reaction by ferric and nickel chloride hexahydrates. One-pot synthesis of 3,4-dihydropyrimidin-2(1H)-ones
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An efficient synthesis of 3,4-dihydropyrimidinones from the aldehyde, β-keto ester and urea in ethanol, using ferric chloride hexahydrate or nickel chloride hexahydrate as the catalyst, is described. Compared with the classical Biginelli reaction conditio
- Lu, Jun,Bai, Yinjuan
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p. 466 - 470
(2007/10/03)
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- A simple and efficient synthesis of 3,4-dihydropyrimidin-2-ones catalysed by amidosulfonic acid
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A general and practical route for the synthesis of dihydropyrimidines by the one-pot cyclocondensation of aldehydes, β-ketoesters and urea is described using NH2SO3H as catalyst. Yields and selectivities are significantly better than
- Jin, Tongshou,Zhang, Suling,Zhang, Suyun,Guo, Junjie,Li, Tongshuang
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- p-toluenesulfonic acid-catalyzed efficient synthesis of dihydropyrimidines: Improved high yielding protocol for the Biginelli reaction
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Dihydropyrimidines are prepared by a one-pot cyclocondensation of aldehydes, β-ketoesters and urea with p-toluenesulfonic acid-catalyzed condensation reaction. Yields are significantly higher than utilizing classical Biginelli reaction conditions.
- Jin, Tongshou,Zhang, Suling,Li, Tongshuang
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p. 1847 - 1851
(2007/10/03)
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- LiClO4-catalyzed one-pot synthesis of dihydropyrimidinones: An improved protocol for Biginelli reaction
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Lithium perchlorate efficiently catalyzes the three-component condensation reaction of aldehyde, β-keto ester and urea in refluxing acetonitrile to afford the corresponding dihydropyrimidinones in high yields under neutral conditions. LiOTf is also found
- Yadav,Subba Reddy,Srinivas,Venugopal,Ramalingam
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p. 1341 - 1345
(2007/10/03)
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- One-pot synthesis of 3,4-dihydropyrimidin-2(1H)-ones using lanthanum chloride as a catalyst
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An efficient synthesis of 3,4-dihydropyrimidinones using lanthanum chloride heptahydrate as a catalyst from an aldehyde, β-keto ester and urea or thiourea in ethanol is described. Compared to the classical Biginelli reaction conditions, this new method co
- Lu,Bai,Wang,Yang,Ma
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p. 9075 - 9078
(2007/10/03)
-